Title : Bupropion binds to two sites in the Torpedo nicotinic acetylcholine receptor transmembrane domain: a photoaffinity labeling study with the bupropion analogue [(125)I]-SADU-3-72.

Pub. Date : 2012 Mar 27

PMID : 22394379






2 Functional Relationships(s)
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1 Based on inhibition of [(125)I]SADU-3-72 binding, SADU-3-72 binds with high affinity (IC(50) = 0.8 muM) to the Torpedo nAChR in the resting (closed channel) state and in the agonist-induced desensitized state, and bupropion binds to that site with 3-fold higher affinity in the desensitized (IC(50) = 1.2 muM) than in the resting state. Bupropion cholinergic receptor nicotinic alpha 4 subunit Homo sapiens
2 These results establish the presence of two distinct bupropion binding sites within the Torpedo nAChR transmembrane domain: a high affinity site at the middle (M2-9) of the ion channel and a second site near the extracellular end of alphaM1 within a previously described halothane (general anesthetic) binding pocket. Bupropion cholinergic receptor nicotinic alpha 4 subunit Homo sapiens